A large number of G-protein-coupled receptors (GPCRs) show varying degrees of basal or constitutive activity. This constitutive activity is usually minimal in natural receptors but is markedly observed in wild type and mutated (naturally or induced) receptors. According to conventional two-state drug receptor interaction model, binding of a ligand may initiate activity (agonist with varying degrees of positive intrinsic activity) or prevent the effect of an agonist (antagonist with zero intrinsic activity). Inverse agonists bind with the constitutively active receptors, stabilize them, and thus reduce the activity (negative intrinsic activity). Receptors of many classes (α-and β-adrenergic, histaminergic, GABAergic, serotoninergic, opiate, and angiotensin receptors) have shown basal activity in suitable in vitro models. Several drugs that have been conventionally classified as antagonists (β-blockers, antihistaminics) have shown inverse agonist effects on corresponding constitutively active receptors. Nearly all H1 and H2 antihistaminics (antagonists) have been shown to be inverse agonists. Among the β-blockers, carvedilol and bucindolol demonstrate low level of inverse agonism as compared to propranolol and nadolol. Several antipsychotic drugs (D2 receptors antagonist), antihypertensive (AT1 receptor antagonists), antiserotoninergic drugs and opioid antagonists have significant inverse agonistic activity that contributes partly or wholly to their therapeutic value. Inverse agonism may also help explain the underlying mechanism of beneficial effects of carvedilol in congestive failure, naloxone-induced withdrawal syndrome in opioid dependence, clozapine in psychosis, and candesartan in cardiac hypertrophy. Understanding inverse agonisms has paved a way for newer drug development. It is now possible to develop agents, which have only desired therapeutic value and are devoid of unwanted adverse effect. Pimavanserin (ACP-103), a highly selective 5-HT2A inverse agonist, attenuates psychosis in patients with Parkinson's disease with psychosis and is devoid of extrapyramidal side effects. This dissociation is also evident from the development of anxioselective benzodiazepines devoid of habit-forming potential. Hemopressin is a peptide ligand that acts as an antagonist as well as inverse agonist. This agent acts as an antinociceptive agent in different in vivo models of pain. Treatment of obesity by drugs having inverse agonist activity at CB1/2 receptors is also underway. An exciting development is evaluation of β-blockers in chronic bronchial asthma—a condition akin to congestive heart failure where β-blockade has become the standard mode of therapy. Synthesis and evaluation of selective agents is underway. Therefore, inverse agonism is an important aspect of drug–receptor interaction and has immense untapped therapeutic potential.

Background: Excessive use of mobile phones, including smart phones, is found to result in various health related, social and psychological problems. Nomophobia expands to ‘No Mobile Phobia’, i.e., fear of being out of mobile phone contact. Previous studies on nomophobia have focused on the student populations, since the younger generation is more technology savvy. This questionnaire-based study aimed to know the prevalence and factors leading to nomophobia in general population.Methods: This study was conducted in western Gujarat from September 2018 to October 2018. A prevalidated questionnaire, containing three parts, the demographic details, details about the characteristics of mobile phone use and the Nomophobia Questionnaire (NMP-Q), was sent through emails and WhatsApp to 1000 individuals. The responses were tabulated and analyzed.Results: Out of 331 respondents 192 (58%) were males and 139 (42%) females. There was no significant difference in average NMP scores with respect to gender (p = 0.401), age brackets (p = 0.135), marital status (p = 0.123) and profession (p = 0.055). However, NMP scores were significantly more in individuals who spent more time on mobile phones per day (p = 0.000), checked their mobile phones more frequently (p<0.000) and in whom phantom ringing syndrome was also present (p<0.000). 241 respondents (72.80%) felt that their mobile phone use was consuming time and affecting their other daily activities.Conclusions: Nomophobia is an emerging health related adverse effect of prolonged mobile phone use. Interventions are required to promote judicious use of mobile phones.

Objectives:The study aims to understand the process and factors influencing the implementation of structured oral examination (SOE) for undergraduate medical students; in comparison with conventional oral examination (COE) in pharmacology.Methods:In a randomized, parallel group study, 123 students of pharmacology were divided into two groups, SOE (n = 63) and COE (n = 60). Students of each group were subdivided into two, and four examiners took viva voce individually. Three sets of questionnaires from autonomic nervous system were prepared, each having 15 items with increasing difficulty levels and were validated by subject experts and pretested. Ten minutes were allotted for each student for each viva. Feedback of students and faculty about the novel method was obtained.Results:SOE yielded significantly lower marks as compared to COE. There were significant inter-examiner variations in marks awarded in SOE and COE. Other factors influencing implementation were difficulty in structuring viva, rigid time limits, lack of flexibility in knowledge content, monotony, and fatigue. The students perceived this format not different from COE but felt that it required in-depth preparation of topic. Faculty opined that SOE led to less drift from main topic and provided uniform coverage of topics in given time.Conclusion:Conducting SOE is a resource-intensive exercise. Despite structuring, inter-examiner variability was not completely eliminated. The students’ performance was depended on factors related to examiners such as teaching experience, vernacular language used, and lack of training. Orientation and training of examiners in assessment strategies is necessary. Standardization of questionnaire is necessary before the implementation of SOE for summative assessment.

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The Medical Council of India (MCI) has formulated a new Competency Based Medical Education (CBME) Curriculum for the Indian Medical Graduates with an objective of making medical education outcome based. A one month long Foundation Course (FC) is a hallmark of this CBME which is implemented during the first month of first professional MBBS studies. The objective is to acquaint, allay apprehension and prepare freshers for further studies using andragogical and heutagogical approaches. The MCI also released the guidelines for the medical colleges for uniform conduct of FC across the country. The FC was divided into six modules, i.e. Orientation Module, Skills Module, Community orientation module, Professional Development and Ethics Module (P and E), Enhancement of Language and Computer Skills Module, and Sports and extracurricular activities.1 A total of 175 hours were allotted to these modules. Like every institute, our institute also developed the implementation program and time-table of FC using MCI guidelines and taking into account the available resources.2,3  The FC at our institute was conducted from 1st August 2019 to 31st August 2019 and was meticulously planned and implemented. The effective implementation  required committed efforts of 30 faculty members (12 Professors, 11 Associate Professors and 7 Assistant Professors), two language and one fine arts teacher,  and 4 non-teaching members  (Librarian, IT-personnel, Coach for sports and motivational Guru). The students were trained to write reflections daily in their log - books which are being analysed further.

Background: This prospective observational study was conducted in a tertiary care hospital in Kachchh, over a period of 6 months, to know the antibiotic sensitivity pattern of pathogens in children less than 18 years old with Urinary Tract Infection (UTI). Methods: Between December 2016 to June 2017, 186 children met the inclusion criterion. Urine samples were collected and processed for urine routine microscopy, culture and antibiotic sensitivity as per the standard laboratory guidelines. Urine culture was positive in 50 cases, which were further evaluated to find out any renal disease. All patients were given 10-14 days antibiotics course and follow-up urine reports were done. Patients were considered cured when the follow-up urine reports were normal. Results: E. coli was the commonest organism (34%) isolated, found mainly in 1-5 years age group (20%). Enterococci were isolated in 32% cases, most of which were less than 5 years of age (28%). Klebsiella (12%), Methicillin Resistant Staphylococcus Aureus (MRSA) (10%), Coagulase negative staphylococci (6%), Pseudomonas (2%) and Budding yeast cell (4%) were the less frequent organisms isolated. E. coli were found to be less sensitive to different Aminoglycosides (11.7% -23.5%), Cephalosporins (11.7% -52.9%), Fluoroquinolones (5.8% -11.7%), Cotrimoxazole (17.6%) and Piperacillin (17.6%), but were more sensitive (70.6%) to Imipenems. Enterococci were also partially sensitive to Aminoglycosides (6.2-18.7%), Cephalosporins (25-37.5.7%), Fluoroquinolones (6.25-12.5%), Penicillin-G (50%), Piperacillin (31.25%) and Co-trimoxazole (43.75%), but had good sensitivity for Imipenems (68.7%), Linezolid (75%) and Vancomycin (81.2%). Similarly, MRSA was 100% sensitive to Linezolid and Imipenem but partially sensitive (20-60%) to other antibiotics. Klebsiella showed 16.65-33.3% sensitivity to all antibiotics except Imipenem (83.3%) and was 100% resistant to Co-trimoxazole. Coagulase negative Staphylococci (CONS) remained 100% sensitive to all antibiotics and Pseudomonas was resistant to all antibiotics. Conclusions: The study concludes that pathogens for UTI in children have developed resistance, even to the newer generation antibiotics, probably due to the irrational use of antibiotics. In view of emergence of multi drug resistant pathogens, which carry considerable morbidity and mortality, every effort must be taken to use antibiotics judiciously.

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Despite availability of a number of oral antidiabetics, a sizeable population of diabetics remains uncontrolled. Thus there is growing need of new group of drugs for diabetic control. Understanding renal conservation of glucose by efficient reabsorption through sodium glucose cotransporter-2 (SGLT-2) has paved way for development of an entirely new group of drugs, the SGLT-2 inhibitors. These glucosuric antidiabetic agents have shown promise in early clinical studies. Canagliflozin is recently approved for use in diabetes alone or along with other antidiabetics. Other highly selective inhibitors undergoing various stages of clinical developments are dapagliflozin, sergliflozin, remogliflozin, ipragliflozin, empagliflozin, luseogliflozin, tofogliflozin and desoxyrhaponticin. KGA-2727 (pyrazole-O-glucoside) is the first selective SGLT-1 inhibitor undergoing intense preclinical testing. There are safety issues associated with this group like urogenital infections (fungal), weight loss, initial osmotic diuresis and increased incidence of cardiovascular events. The long term safety remains to be established. Despite these limitations, SGLT-2 inhibition offers a unique target for achieving adequate control of diabetes in adults. [Int J Basic Clin Pharmacol 2013; 2(4.000): 347-352